A new, specific, rapid gas chromatography-mass spectrometry (GC-MS) method was described to identify and quantify pregabalin in human plasma. Silylation and acylation reaction were tried for derivatization of pregabalin before GC-MS analysis. Derivatization was achived using N-(tert-butyldimethylsilyl)-N-methyltrifluoroacetamide (MTBSTFA). Identification and quantification of a new derivative were performed in selected ion monitoring mode using electron impact ionization. Pregabalin was extracted from plasma by protein precipitation with acetonitrile. The extraction recovery ranged from 60.23-73.19 %. The GC-MS method was validated and the validation parameters; specificity, limit of quantitation (LOQ) and detection (LOD), linearity, recovery,
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Introduction
Pregabalin (isobutyl γ-aminobutyric acid; (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid) is an antiepileptic drug. It was authorized in 2004 in Europe and 2005 in the United States for the adjunctive treatment of partial seizures in adult epilepsy patients [1]. However, nearly all of its use is for patients with neuropathic pain [2,3].
Pregabalin binds to the 2- subunit, an auxiliary protein, of Q-type voltage-sensitive calcium channels and modulates calcium channel traffic and physiology thus reducing the presynaptic calcium influx and subsequent neurotransmitter release [1].
After oral administration, pregabalin is well absorbed and reaches the peak plasma concentration (Cmax) between 0.7 and 1.3 hours [4]. Its oral bioavailability is approximately 90% and is independent of dose. Food consumption can reduce Cmax by 25–30%, and increase the time to maximum peak plasma concentration to 3 hours [5]. Pregabalin is eliminated almost by renal excretion. Its metabolism in liver is negligible and is not bound to plasma proteins [6]
Analytical methods for the analysis of pregabalin in biological samples are required to understand its pharmacokinetic profile among various patients, to compare bioavailability of pharmaceutical formulations of pregabalin and to determine therapeutic concentration in patients …show more content…
It was monitored ultraviolet (UV) [9,12-14], fluorescence (FL) [10,11,15] and tandem mass spectrometry (MS-MS) [16-23] detector. Pregabalin lacks of specific UV chromophore group so it doesn’t give characteristic UV spectra. Nevertheless, there have been reported studies performed UV detection at 200, 210 nm [9,12]. In some studies, post-column or pre-column derivatization step was applied to increase specificity and sensitivity of the analytical methods
Introduction
Pregabalin (isobutyl γ-aminobutyric acid; (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid) is an antiepileptic drug. It was authorized in 2004 in Europe and 2005 in the United States for the adjunctive treatment of partial seizures in adult epilepsy patients [1]. However, nearly all of its use is for patients with neuropathic pain [2,3].
Pregabalin binds to the 2- subunit, an auxiliary protein, of Q-type voltage-sensitive calcium channels and modulates calcium channel traffic and physiology thus reducing the presynaptic calcium influx and subsequent neurotransmitter release [1].
After oral administration, pregabalin is well absorbed and reaches the peak plasma concentration (Cmax) between 0.7 and 1.3 hours [4]. Its oral bioavailability is approximately 90% and is independent of dose. Food consumption can reduce Cmax by 25–30%, and increase the time to maximum peak plasma concentration to 3 hours [5]. Pregabalin is eliminated almost by renal excretion. Its metabolism in liver is negligible and is not bound to plasma proteins [6]
Analytical methods for the analysis of pregabalin in biological samples are required to understand its pharmacokinetic profile among various patients, to compare bioavailability of pharmaceutical formulations of pregabalin and to determine therapeutic concentration in patients …show more content…
It was monitored ultraviolet (UV) [9,12-14], fluorescence (FL) [10,11,15] and tandem mass spectrometry (MS-MS) [16-23] detector. Pregabalin lacks of specific UV chromophore group so it doesn’t give characteristic UV spectra. Nevertheless, there have been reported studies performed UV detection at 200, 210 nm [9,12]. In some studies, post-column or pre-column derivatization step was applied to increase specificity and sensitivity of the analytical methods